Novel Hybrid Molecules of Isoxazole Chalcone Derivatives: Synthesis and Study of in vitro Cytotoxic Activities

Publisher: Bentham Science Publishers

E-ISSN: 1875-628x|15|6|576-582

ISSN: 1570-1808

Source: Letters in Drug Design & Discovery, Vol.15, Iss.6, 2018-04, pp. : 576-582

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Abstract

Background: Now-a-days, the model of “hybrid drugs” has acquired recognition inmedicine due to their significant role in the treatment of different health problems.

Methods: We have synthesized new series of isoxazole-chalcone conjugates (14a-m) by theClaisen-Schmidt condensation of suitable substituted acetophenones with isoxazole aldehydes (12a-d).In vitro cytotoxic activity of the synthesized compounds was studied against four different selectedhuman cancer cell lines by using sulforhodamine B (SRB) method.

Results: The adopted scheme resulted in good yields of new series of isoxazole-chalconeconjugates (14a-m). Potent cytotoxic activity was observed for compounds -14a, 14b, 14e, 14i, 14jand 14k against prostate DU-145 cancer cell line.

Conclusion: The observed potent cytotoxic activities were due to the presence of 3,4,5-trimethoxyphenyl group.